40478-49-7

Upstream product

• 10516-71-9 3-(3-Methoxy-phenyl)-propionic acid 
• 591-31-1 3-methoxy-benzaldehyde 
• 6099-04-3 3-methoxycinnamic acid 
• 6099-04-3 trans-3-methoxycinnamic acid 

Downstream Products

• 73706-63-5 1-Diazo-4-(3-methoxyphenyl)butan-2-one 
• 78649-10-2 3-amino-2-<2-(3-methoxyphenyl)ethyl>quinazolin-4(3H)-one 
• 83988-42-5 methyl N-<3-(3-methoxyphenyl)propanoyl>anthranilate 
• 6968-35-0 7-hydroxy-indan-1-one 
• 5111-70-6 5-methoxy-1-indanone 
• 372516-06-8 N-benzyl-N-(2,2-dimethyl-4H-[1,3]dioxin-5-yl)-3-(3-methoxy-phenyl)-propionamide 
• 837362-59-1 5-(3-methoxtphenyl)-1-(trimethylsilyl)pent-3-yn-2-one 
• 871905-79-2 (5R,6R)-5-Benzyl-1-[3-(3-methoxy-phenyl)-propionyl]-6-(2-trimethylsilanyl-ethoxymethoxy)-[1,2,4]triazepan-3-one 
• 1190732-16-1 N-(4,4-diethoxybutyl)-3-(3-methoxy-phenyl)propionamide 
• 1227263-11-7 N-(2-methoxyphenyl)-3-(3-methoxyphenyl)propanamide 
• 1267276-53-8 1,1,1-trifluoro-4-(3-methoxyphenyl)butan-2-one 
• 1386380-38-6 N,N-bis(2-cyano-5-methoxyphenyl)-3-(3-methoxyphenyl)propanamide 
• 585569-12-6 C₁₆H₁₈O₆ 

Relevant academic research and scientific papers

Kinetics-Driven Drug Design Strategy for Next-Generation Acetylcholinesterase Inhibitors to Clinical Candidate

The acetylcholinesterase (AChE) inhibitors remain key therapeutic drugs for the treatment of Alzheimer's disease (AD). However, the low-safety window limits their maximum therapeutic benefits. Here, a novel kinetics-driven drug design strategy was employed to discover new-generation AChE inhibitors that possess a longer drug-target residence time and exhibit a larger safety window. After detailed investigations, compound 12 was identified as a highly potent, highly selective, orally bioavailable, and brain preferentially distributed AChE inhibitor. Moreover, it significantly ameliorated cognitive impairments in different mouse models with a lower effective dose than donepezil. The X-ray structure of the cocrystal complex provided a precise binding mode between 12 and AChE. Besides, the data from the phase I trials demonstrated that 12 had good safety, tolerance, and pharmacokinetic profiles at all preset doses in healthy volunteers, providing a solid basis for its further investigation in phase II trials for the treatment of AD.

Ruthenium-catalyzed intramolecular arene C(sp2)-H amidation for synthesis of 3,4-dihydroquinolin-2(1 H)-ones

We report the [Ru(p-cymene)(l-proline)Cl] ([Ru1])-catalyzed cyclization of 1,4,2-dioxazol-5-ones to form dihydroquinoline-2-ones in excellent yields with excellent regioselectivity via a formal intramolecular arene C(sp2)-H amidation. The reactions of the 2- and 4-substituted aryl dioxazolones proceeds initially through spirolactamization via electrophilic amidation at the arene site, which is para or ortho to the substituent. A Hammett correlation study showed that the spirolactamization is likely to occur by electrophilic nitrenoid attack at the arene, which is characterized by a negative ρ value of -0.73.

Copper-Catalyzed Oxidative Benzylic C(sp3)?H Cyclization for the Synthesis of β-Lactams

β-Lactams are important structural motifs because of their ubiquity in natural products and pharmaceuticals. We report herein a Cu-catalyzed intramolecular oxidative C(sp3)?H amidation for the synthesis of β-lactams using tBuOOtBu. This method

Rh(III)-Catalyzed meta-C-H Olefination Directed by a Nitrile Template

A range of Rh(III)-catalyzed ortho-C-H functionalizations have been developed; however, extension of this reactivity to remote C-H functionalizations through large-ring rhodacyclic intermediates has yet to be demonstrated. Herein we report the first examp

GluN2B-selective N-methyl-d-aspartate (NMDA) receptor antagonists derived from 3-benzazepines: Synthesis and pharmacological evaluation of benzo[7]annulen-7-amines

Given their high neuroprotective potential, ligands that block GluN2B-containing N-methyl-D-aspartate (NMDA) receptors by interacting with the ifenprodil binding site located on the GluN2B subunit are of great interest for the treatment of various neurona

ANTI-CANCER ACTIVITY OF NOVEL BICYCLIC HETEROCYCLES

The present invention relates to compound of formula I, II, III, or IV, and/or a pharmaceutical acceptable addition salt thereof and/or a stereoisomer thereof and/or a solvate thereof, Formulas (I), (II), (III) and (IV) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R11, and R12 are as defined in the claim 1 or as described in detail in the description of the invention, and to the use of said compounds to treat or prevent proliferative disorders and their use to manufacture a medicine to treat or prevent proliferative disorders, particularly cancer such as leukemia. The present invention also relates to pharmaceutical compositions of said compounds and the use of said pharmaceutical compositions to treat or prevent proliferative disorders. The present invention further relates to the use of said compounds as biologically active ingredients, more specifically as medicaments for the treatment of proliferative disorders and pathologic conditions such as, but not limited to, cancer such as leukemia.

Thieno[2,3-d]pyrimidine-2-carboxamides bearing a carboxybenzene group at 5-position: Highly potent, selective, and orally available MMP-13 inhibitors interacting with the S1″ binding site

On the basis of X-ray co-crystal structures of matrix metalloproteinase-13 (MMP-13) in complex with its inhibitors, our structure-based drug design (SBDD) strategy was directed to achieving high affinity through optimal protein-ligand interaction with the unique S1″ hydrophobic specificity pocket. This report details the optimization of lead compound 44 to highly potent and selective MMP-13 inhibitors based on fused pyrimidine scaffolds represented by the thienopyrimidin-4-one 26c. Furthermore, we have examined the release of collagen fragments from bovine nasal cartilage in response to a combination of IL-1 and oncostatin M.

Cross-coupling of remote meta -c-h bonds directed by a u-shaped template

meta-C-H arylation and methylation of 3-phenylpropanoic acid and phenolic derivatives were developed using an easily removable nitrile template. The combination of a weakly coordinating U-shaped template and mono-protected amino acid ligand was crucial fo

Superacid-catalyzed Friedel-Crafts cyclization of unactivated alkenes

Trifluoromethanesulfonimide is an effective catalyst for Friedel-Crafts cyclizations of simple, nonpolarized alkenes with a variety of pendant arenes. A catalyst loading of 0.5 - 1.0 mol % effects clean cyclization to form 5- to 7-membered carbocycles wit

Design and optimization of potent and orally bioavailable tetrahydronaphthalene raf inhibitors

Inhibition of mutant B-Raf signaling, through either direct inhibition of the enzyme or inhibition of MEK, the direct substrate of Raf, has been demonstrated preclinically to inhibit tumor growth. Very recently, treatment of B-Raf mutant melanoma patients with a selective B-Raf inhibitor has resulted in promising preliminary evidence of antitumor activity. This article describes the design and optimization of tetrahydronaphthalene-derived compounds as potent inhibitors of the Raf pathway in vitro and in vivo. These compounds possess good pharmacokinetic properties in rodents and inhibit B-Raf mutant tumor growth in mouse xenograft models.